Anticonvulsant activities of α-asaronol (( E )-3′-hydroxyasarone), an active constituent derived from α-asarone

He, Xirui; Bai, Yajun; Zhang, Min; Zhao, Zhengyan; Qiang, Zhang; Xu, Ning; Qin, Fanggang; Wei, Xiaoyang; Zhao, Meimei; Wu, Na; Li, Zehua; Zhang, Yajun; Fan, Tai-Ping; Zheng, Xiaohui

doi:10.1016/j.pharep.2017.08.004

Cited by 23 publications

(25 citation statements)

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“…The anticonvulsant effects of α-asaronol ((E)-3’-hydroxyasarone), an active constituent derived from α-asarone, were assessed in an in vivo anticonvulsant screening assay using the three most commonly employed mouse models of seizure, including 3-mercaptopropionic-acid (3-MP)-induced seizures, maximal-electroshock seizures (MES), and subcutaneous-injection-pentylenetetrazole (PTZ)-induced seizures [ 189 ]. The oral administration of α-asaronol resulted in a broad spectrum of anticonvulsant activity and displayed better protective indices (PI = 11.11 in MES mice and PI = 8.68 in PTZ mice) and lower acute toxicity (LD 50 = 2940 mg/kg) than its metabolic parent compound (α-asarone).…”

Section: Neuroprotective Effects Of α- and β-Asarone On Other Neurolo...mentioning

confidence: 99%

Molecular Mechanisms and Therapeutic Potential of α- and β-Asarone in the Treatment of Neurological Disorders

et al. 2022

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Neurological disorders are important causes of morbidity and mortality around the world. The increasing prevalence of neurological disorders, associated with an aging population, has intensified the societal burden associated with these diseases, for which no effective treatment strategies currently exist. Therefore, the identification and development of novel therapeutic approaches, able to halt or reverse neuronal loss by targeting the underlying causal factors that lead to neurodegeneration and neuronal cell death, are urgently necessary. Plants and other natural products have been explored as sources of safe, naturally occurring secondary metabolites with potential neuroprotective properties. The secondary metabolites α- and β-asarone can be found in high levels in the rhizomes of the medicinal plant Acorus calamus (L.). α- and β-asarone exhibit multiple pharmacological properties including antioxidant, anti-inflammatory, antiapoptotic, anticancer, and neuroprotective effects. This paper aims to provide an overview of the current research on the therapeutic potential of α- and β-asarone in the treatment of neurological disorders, particularly neurodegenerative diseases such as Alzheimer’s disease (AD), Parkinson’s disease (PD), as well as cerebral ischemic disease, and epilepsy. Current research indicates that α- and β-asarone exert neuroprotective effects by mitigating oxidative stress, abnormal protein accumulation, neuroinflammation, neurotrophic factor deficit, and promoting neuronal cell survival, as well as activating various neuroprotective signalling pathways. Although the beneficial effects exerted by α- and β-asarone have been demonstrated through in vitro and in vivo animal studies, additional research is required to translate laboratory results into safe and effective therapies for patients with AD, PD, and other neurological and neurodegenerative diseases.

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Section: Neuroprotective Effects Of α- and β-Asarone On Other Neurolo...mentioning

confidence: 99%

Molecular Mechanisms and Therapeutic Potential of α- and β-Asarone in the Treatment of Neurological Disorders

et al. 2022

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“…Therefore, the research on epilepsy and its treatment has extremely important practical signi cance and urgency. At present, the major choice for the treatment of epilepsy in the clinic is still mainly drugs (He et al 2018). However, the existing clinical antiepileptic drugs (AEDs) are only about 2/3 of epileptic patients achieve a satisfactory seizure control, and the treatment effect is poor or ineffective for the other 1/3 of epileptic patients (He et al 2018; Kondrat-Wróbel and Łuszczki, 2018; Bai et al 2019).…”

Section: Introductionmentioning

confidence: 99%

“…At present, the major choice for the treatment of epilepsy in the clinic is still mainly drugs (He et al 2018). However, the existing clinical antiepileptic drugs (AEDs) are only about 2/3 of epileptic patients achieve a satisfactory seizure control, and the treatment effect is poor or ineffective for the other 1/3 of epileptic patients (He et al 2018; Kondrat-Wróbel and Łuszczki, 2018; Bai et al 2019). Currently available antiepileptic drugs can also not prevent the development of epilepsy drug resistance, which is considered to be a challenge in epilepsy treatment.…”

Section: Introductionmentioning

confidence: 99%

“…3-MP-induced seizures test were carried out according to previously described methods(He et al 2018;Bai et al 2019). Elevated plus mazeThe elevated plus maze (EPM) is a simple method to assess anxiety-like behaviors in mice by estimating contradictory and con icting behavior between the exploring characteristics of animals to new/different environments and the fear of hanging open arms forms (Guillén-Ruiz et al 2021).…”

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confidence: 99%

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Evaluation of the Anticonvulsant Activities of Gastrodia Elata Bl.- Acorus Tatarinowii Decoction on Experimentally Induced Seizures in Mice

Yang

Yuan

et al. 2022

Preprint

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Epilepsy is a serious public health problem in the world. At present, the effect of drug treatment of epilepsy is are not satisfactory. Medicinal plants as pharmaceuticals and for healthcare treatments in the management of epilepsy in China for many centuries. Especially, Gastrodia elata Bl.-Acorus tatarinowii, as a classic and important herb pairs in folk medicine, has been used in folk medicine to control seizures. However, the animal experiment data of its anticonvulsant effect is limited in the literature. The objective of this study was to mainly analyze the anticonvulsant activity of Gastrodia elata-Acorus tatarinowii (GEAT) decoction in maximal electroshock (MES), pentylenetetrazole (PTZ) and trimercaptopropionic acid (3-MP) induced seizures in mice, providing scientific basis for the treatment of convulsive disorders in traditional medicine. In addition, the improvement effect were examined on seizure severity, anxiety, cognitive dysfunction, inflammation and oxidative stress in PTZ kindled mice. The results showed that GEAT decoction dose-dependently protected mice against MES, 3-MP and PTZ induced acute seizures. Meanwhile, GEAT decoction ameliorated seizure severity, decreased the accumulation of inflammatory mediators TNF-α, IL-1β, and IL-6, mitigated oxidative stress, as well as alleviated anxious-like behavior and cognitive deficits in PTZ-kindled mice. Our data evidenced that the anticonvulsant properties attributed to GEAT decoction as adjunctive therapy for epileptic patients in folk medicine.

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“…2), which means to integrate active constituents based on TCM theory. Accordint to the strategy CTCMC, we have developed potential lead compounds including DBZ (tanshinol borneol ester) [14,15], 2hydroxypyrrolobenzodiazepine-5,11-dione analogues [16] and TMCA-a-asaronol ester [17,18]. We believe that this strategy is benefit to the innovation of new drugs from natural products.…”

Section: Introductionmentioning

confidence: 99%

Research progress in the biological activities of 3,4,5-trimethoxycinnamic acid (TMCA) derivatives

Zhao

Song

Xie

et al. 2019

European Journal of Medicinal Chemistry

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a b s t r a c t TMCA (3,4,5-trimethoxycinnamic acid) ester and amide are privileged structural scaffolds in drug discovery which are widely distributed in natural products and consequently produced diverse therapeutically relevant pharmacological functions. Owing to the potential of TMCA ester and amide analogues as therapeutic agents, researches on chemical syntheses and modifications have been carried out to druglike candidates with broad range of medicinal properties such as antitumor, antiviral, CNS (central nervous system) agents, antimicrobial, anti-inflammatory and hematologic agents for a long time. At the same time, SAR (structure-activity relationship) studies have draw greater attention among medicinal chemists, and many of the lead compounds were derived for various disease targets. However, there is an urgent need for the medicinal chemists to further exploit the precursor in developing chemical entities with promising bioactivity and druggability. This review concisely summarizes the synthesis and biological activity for TMCA ester and amide analogues. It also comprehensively reveals the relationship of significant biological activities along with SAR studies.

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Anticonvulsant activities of α-asaronol (( E )-3′-hydroxyasarone), an active constituent derived from α-asarone

Cited by 23 publications

References 26 publications

Molecular Mechanisms and Therapeutic Potential of α- and β-Asarone in the Treatment of Neurological Disorders

Molecular Mechanisms and Therapeutic Potential of α- and β-Asarone in the Treatment of Neurological Disorders

Evaluation of the Anticonvulsant Activities of Gastrodia Elata Bl.- Acorus Tatarinowii Decoction on Experimentally Induced Seizures in Mice

Research progress in the biological activities of 3,4,5-trimethoxycinnamic acid (TMCA) derivatives

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